Document Detail


Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
MedLine Citation:
PMID:  18507366     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
D-amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including d-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[ d]isoxazol-3-ol derivatives were synthesized and evaluated as DAAO inhibitors. Among them, 5-chloro-benzo[ d]isoxazol-3-ol (CBIO) potently inhibited DAAO with an IC50 in the submicromolar range. Oral administration of CBIO in conjunction with d-serine enhanced the plasma and brain levels of d-serine in rats compared to the oral administration of d-serine alone.
Authors:
Dana Ferraris; Bridget Duvall; Yao-Sen Ko; Ajit G Thomas; Camilo Rojas; Pavel Majer; Kenji Hashimoto; Takashi Tsukamoto
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-05-29
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  51     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2008 Jun 
Date Detail:
Created Date:  2008-06-19     Completed Date:  2008-09-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  3357-9     Citation Subset:  IM    
Affiliation:
MGI Pharma, Inc.
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Animals
Benzoxazoles / chemical synthesis*,  chemistry,  pharmacology
Brain / metabolism
D-Amino-Acid Oxidase / antagonists & inhibitors*
Drug Synergism
Isoxazoles / chemical synthesis*,  chemistry,  pharmacology
Male
Rats
Rats, Sprague-Dawley
Serine / administration & dosage,  metabolism,  pharmacology
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/5-chlorobenzo(d)isoxazol-3-ol; 0/Benzoxazoles; 0/Isoxazoles; 56-45-1/Serine; EC 1.4.3.3/D-Amino-Acid Oxidase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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